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用对氟苯甲醛为原料经Wittig反应,Sharpless不对称环氧化和环氧的区域性开环等反应合成了R-和S-β-对氟苯基乳酸及其甲醛,并测定和确定了它们的光学纯度和绝对构型。经初步药理实验结果表明:S-β-对氟苯基乳酸抑制血小板聚集能力比R-β-对氟苯基乳酸强,它们的甲酯化合物抑制血小板聚集能力更强。
R- and S-β-p-fluorophenyl lactic acid and formaldehyde were synthesized from p-fluorobenzaldehyde via Wittig reaction, Sharpless asymmetric epoxidation and the ring-opening reaction of epoxy. Their optical purity and absolute configuration. The results of preliminary pharmacological experiments show that S-β-p-fluorophenyl lactic acid has stronger ability to inhibit platelet aggregation than R-β-p-fluorophenyl lactic acid, and their methyl ester compounds inhibit platelet aggregation stronger.